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Prostate-specific membrane antigen (PSMA) theranostics offers a new approach for a personalized and targeted treatment for metastatic prostate cancer. Lutetium-177-labelled PSMA-ligands (177Lu-PSMA) is a radionuclide therapy that is directed to PSMA expressing prostate cancer. Clinical experience with 177Lu-PSMA in men with advanced prostate cancer is growing. The purpose of this review is to outline the mechanism of action of this therapy, summarize recent efficacy and toxicity data and highlight future direction and challenges in establishing 177Lu-PSMA treatment as part of routine clinical practice.The first reports on safety and efficacy of 177Lu-PSMA have been retrospective series of men with advanced prostate cancer who previously failed conventional therapies and received 177Lu-PSMA on compassionate basis. These studies highlight promising efficacy, favourable toxicity profile and quality of life improvements. Limitation stem from the retroospective nature of these data with short follow-up.Several studies suggest that radionuclide therapy with 177Lu-PSMA has high activity and is well tolerated. Crucial to establishing this treatment in routine clinical management will be the generation of high-level evidence from prospective trials that can confirm the encouraging patient outcomes reported to date.